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Prior art relating to this invention concerns distinct areas previously not combined to create new and useful formula sets regarding a solid-dosage form of a weight loss product.
This invention relates a new and unique combination of octopamine, yohimbine, bergenin and decaffeinated green tea extract useful for increasing weight loss.
Octopamine is a naturally-occurring catecholamine structurally related to norephinephrine, and has been proven in in-vitro studies to be a potent selective beta-3 agonist (C R Acad Sci III 1993;316(5):519-23). Beta-3 receptors can be found in both human white and brown adipose tissues, and play an important role in lipolysis and thermogenesis in our bodies. They are vastly more important than previously thought by scientists, who often had difficulty in the past discerning the contribution of each beta-receptor subtype (1,2 and 3) without having agents selective for each to investigate. Various techniques were devised to try, but for a long time reports were not in favor of beta-3 receptors having much of a role in humans. It was not until a study conducted with ephedrine in 1995, however, that surprising new data started to arise in support of a beta-3-mediated pathway to fat loss. Using beta blocking agents investigators were able to demonstrate that beta-3 agonist activity likely accounted for at least 40% of the thermogenesis induced by this popular weight loss drug.
When a synthetic selective beta-3 agonist was finally developed and studied in humans in 2001, the important role of this receptor became an unquestionable fact (Clin Pharmacol Ther 2002;71:272-9). In this investigation a group of 12 otherwise healthy overweight men noticed a clear increase in lipolysis, as well as total energy expenditure, with the use of a beta-3 agonist exclusively. We are sure the intended action of the drug was solely responsible for these effects because heart-rate and diastolic blood pressure did not increase in any of the subjects (signs that non-selective beta agonistic activity were occurring), nor did the concentrations of the endogenous adrenergic hormones epinephrine and norepinephrine. Leptin, a hormone often relevant to weight loss, also did not change during the study. We are left with proof that beta-3 receptors are important triggers of lipolysis and thermogenesis in humans, and have opened a new door to weight loss without the uncomfortable jitters and central nervous system stimulation noted with non-selective beta agonists like ephedrine (selective beta-3 agonists do not produce the same strong CNS stimulation).
Yohimbine is an extremely potent naturally-occurring alpha-2 receptor antagonist. Adrenergic lipolysis in human adipose tissue is regulated in a dual nature by adrenoceptors. Most notably, activation of the beta-2 or beta-3 subtype increases the process of lipolysis; while activation of alpha-2 receptors diminishes it (fat cells appear to be the only type of cells in the human body that exhibit such dual regulation by adrenoceptors). Studies with yohimbine, in the form of yohimbine HCL, have shown that it is capable of increasing lipolysis in humans after oral dosing, likely via both alpha-2 receptor antagonism and increases in synaptic norephinephrine release (Eur J Clin Invest 1988;18:587-94). In effect it serves both beta stimulating and alpha blocking properties, an ideal combination if we want to stimulate fat loss. However, when single doses as high as 21.6 mg (J Clin Pharmacol 1996;36:814-22), or daily cumulative doses as high as 43.2 mg (J Urol 1995;141:1360-63), were taken, the agent was well tolerated, and had no significant impact on blood pressure or heart rate as would be expected of a beta-agonist like ephedrine.
Green tea leaf (camellia sinensis) extract has been around for centuries, and has been used in herbal medicine for about as long. Early on its beneficial properties were noticed, particularly in Asian cultures where Green Tea has been widely consumed and often thought of as a having numerous positive health benefits. In recent years scientists have been investigating the content and actions of Green Tea, and are coming to confirm with solid evidence many of its positive effects including those as an anti-oxidant, cholesterol lowering, antidepressant, capillary-strengthening and lipolysis-enhancing agent. Early suggestions were that its caffeine content was solely responsible for its ability to increase fat loss; however this was fundamentally dismissed in a study published in 1999 that demonstrated green tea to have an effect that could not be duplicated with an equivalent dose (50 mg) of caffeine (Int J Obesity 2000;24:252-58). In this investigation green tea increased 24 hour energy expenditure significantly, where the caffeine had no noticeable effect. It looks now like its high content of tea-catechins, particularly EGCG, which are the source of its activity here. Studies with Green Tea extract with standardized amounts of EGCG have suggested it exerts a direct effect on thermogenesis by increasing the respiration rate of brown fat cells, and furthermore that it can strongly enhance the lipolytic action of other chemicals or agents acting on this system (Am J Clin Nutr 1999;70:1040-5). In-vitro tea catechins like EGCG were shown to inhibit the COMT enzyme, which is responsible for degrading the adrenergic hormone norephinephrine (J Med Chem 1975;18:120-2). Since norepinephrine has an important role in human thermogenesis and fat metabolism, this likely accounts for much of its positive action here.
Bergenin comes from eastern herbal medicine originally, where it is found in the form of a plant extract called xe2x80x9cShengmaxe2x80x9d. It is one of the now known active components of this plant extract, and has been shown to have an action in the body that augments the lipolytic action of norepinephrine. In-vitro studies have confirmed that while this compound itself does not directly stimulate lipolysis or have measurable adrenergic activity, but it markedly enhances lipolysis enduced by an adrenergic hormone such as norepinephrine (J. Nat Prod 1998;61:1006-11). It is further documented to oppose the lipogenic (fat building) actions of insulin. Its exact mode of action is unknown at this time, but it is believed to involve increased norepinephrine binding affinity to phosholipids on fat cells.
By triggering adrenergically-mediated lipolysis and thermogenesis with a carefully blended combination of octopamine and yohimbine, while simultaneously supporting the adrenergically-mediated activities of these compounds with a carefully blended composition of bergenin and decaffeinated green tea extract, this new product provides a unique and effective method for losing weight.
Prior art relates many dietary supplement formulations for the purpose of increasing weight loss. Many, however, focus on the use of strong central nervous system stimulants such as caffeine and ephedrine (or its alkaloids). Although effective in many cases, stimulant-based weight loss products are often uncomfortable for many users due to the side effects related to their potential effects on the central nervous system, which may include restlessness, increased heart rate, sweating or insomnia. Prior art also discloses four compounds of interest to this inventor that are without strong stimulant properties, but which heretofore had not been combined to create a new and useful weight loss product. The problem of this invention was therefore to provide a new and unique composition for increasing weight loss in humans, but without the use of strong stimulants. According to this invention this problem is solved with a carefully blended composition containing octopamine, yohimbine, bergenin and decaffeinated green tea extract.
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